| Design and synthesis of novel inhibitors of human kynurenine aminotransferase-I. | |
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MedLine Citation:
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PMID: 22281190 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1H-indole-2-carboxylic acid derivatives as synthetically accessible leads for human kynurenine aminotransferase-I (KAT-I) inhibitors. In total, 12 compounds were synthesized and their biological activities were determined using the HPLC-UV based KAT-I inhibition assay. Of the 12 compounds synthesized, 10 were found to inhibit human KAT-I and the most active compound was found to be 5-(2-(4-chlorophenyl) hydrazono)-6-ethoxy-6-oxohexanoic acid (9a) with an IC(50) of 19.8μM. |
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Authors:
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Fady N Akladios; Naveed A Nadvi; Joohong Park; Jane R Hanrahan; Vimal Kapoor; Mark D Gorrell; W Bret Church |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-1-10 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2012 Jan |
Date Detail:
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Created Date: 2012-1-27 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012 Elsevier Ltd. All rights reserved. |
Affiliation:
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Faculty of Pharmacy A15, The University of Sydney, Sydney NSW 2006, Australia. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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